蛋白质水解
生物
效应器
药物发现
计算生物学
癌症研究
生物信息学
酶
免疫学
生物化学
作者
Xi‐Chun M. Lu,Jinmei Jin,Ye Wu,Xiaoxia Liu,Xiaohui Liang,Jiayi Lin,Qian Sun,Jiang‐Jiang Qin,Guoqing Zhang,Xin Luan
摘要
As a widely considerable target in chemical biology and pharmacological research, rat sarcoma (RAS) gene mutations play a critical driving factor in several fatal cancers. Despite the great progress of RAS subtype-specific inhibitors, rapid acquired drug resistance could limit their further clinical applications. Proteolysis targeting chimera (PROTAC) has emerged as a powerful tool to handle "undruggable" targets and exhibited significant therapeutic benefit for the combat of drug resistance. Owing to unique molecular mechanism and binding kinetics, PROTAC is expected to become a feasible strategy to break the bottleneck of classical RAS inhibitors. This review aims to discuss the current advances of RAS inhibitors and especially focus on PROTAC strategy targeting RAS mutations and their downstream effectors for relevant cancer treatment.
科研通智能强力驱动
Strongly Powered by AbleSci AI